Dolastatin 10
(Synonyms: DLS 10; NSC 376128) 目录号 : GC16273
Dolastatin 10 (DLS 10) 是一种有效的抗有丝分裂肽，可抑制微管蛋白聚合。
Cas No.:110417-88-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Dolastatin 10 is an antitumor agent [1].
Dolastatin 10 is a potent antimitotic polypeptide isolated from a marine animal and is developed as a potential antitumor agent. Dolastatin 10 is found to have activity to inhibit tubulin polymerization with IC50 value of 1.2μM. Besides that, it potently inhibits vincristine binding to tubulin with a Ki value of 1.4μM in a noncompetitive manner. Dolastatin 10 also shows moderate effect on enhancing the binding of colchicines to tubulin. In addition, Dolastatin 10 has the inhibitory activity in tubulin-dependent GTP binding [1].
In the cellular assay, Dolastatin 10 shows activity against some human leukaemia, lymphoma and solid tumour cell lines (such as OVCAR-3 and NSCLC) with IC50 values ranging from 0.1nM to 10nM. It is currently tested in the clinical trials [2].
References:
[1] Bai R L, Pettit G R, Hamel E. Binding of dolastatin 10 to tubulin at a distinct site for peptide antimitotic agents near the exchangeable nucleotide and vinca alkaloid sites. Journal of Biological Chemistry, 1990, 265(28): 17141-17149.
[2] Schwartsmann G. Marine organisms and other novel natural sources of new cancer drugs. Annals of Oncology, 2000, 11(suppl 3): 235-243.
| Cas No. | 110417-88-4 | SDF | |
| 别名 | DLS 10; NSC 376128 | ||
| 化学名 | (2S)-2-[[(2R)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3S,4S)-3-methoxy-1-[(2S)-2-[(1R,2S)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide | ||
| Canonical SMILES | CCC(C)C(C(CC(=O)N1CCCC1C(C(C)C(=O)NC(CC2=CC=CC=C2)C3=NC=CS3)OC)OC)N(C)C(=O)C(C(C)C)NC(=O)C(C(C)C)N(C)C | ||
| 分子式 | C42H68N6O6S | 分子量 | 785.09 |
| 溶解度 | ≥ 78.5mg/mL in EtOH | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2737 mL | 6.3687 mL | 12.7374 mL |
| 5 mM | 0.2547 mL | 1.2737 mL | 2.5475 mL |
| 10 mM | 0.1274 mL | 0.6369 mL | 1.2737 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。